ArticleProceedings of the National Academy of Sciences of the United States of America2012
Phenanthriplatin, a monofunctional DNA-binding platinum anticancer drug candidate with unusual potency and cellular activity profile.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 98 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
98 citing papers in PubMed, 317 citations in OpenAlex.
- Recent trends of organic synthesis through cobalt metal-based catalysis: a review.RSC advances · 2026Review
- Evaluation of the Cytotoxic and Antimigratory Activity Induced by [Pt(1-hexyl-1International journal of molecular sciences · 2026Article
- Computational Analysis of Chromophore-Controlled Photoactivation in Monofunctional Platinum(II)-BODIPY Conjugates for Dual Chemo-Photodynamic Therapy.Chembiochem : a European journal of chemical biology · 2026Article
- A whole genomic CRISPR-Cas9 screen identifies the amino acid transporter SLC43A1 (LAT3) as a major determinant of oxaliplatin sensitivity in colorectal cancer cells.Molecular cancer therapeutics · 2026Article
- Cytotoxicity and antimicrobial activity of platinum(II) complexes based on the ligand precursor 2-phenyl-6-(1,2,3-triazol-4-yl)pyridine - influence of substituent and ancillary ligand on selectivity and activity.Zeitschrift fur Naturforschung. C, Journal of biosciences · 2026Article
- The role of cisplatin in modulating the tumor immune microenvironment and its combination therapy strategies: a new approach to enhance anti-tumor efficacy.Annals of medicine · 2025Review
- The grinding route for synthesis of dihydropyrrolophenanthrolines and their conversion to dipyrrolophenanthrolines under reflux condition.Scientific reports · 2025Article
- Leveraging platinum-protein interactions to overcome chemoresistance.Nature communications · 2025Article
- Thermoresponsive Hyaluronate-Based Nanogels for Enhanced Phenanthriplatin Delivery in Cisplatin-Resistant Ovarian Cancer.Biomacromolecules · 2025Article
- Reimagining Pt(II) Anticancer Agents: The Role of Ferrocene in Monofunctional Chemotherapeutic Compounds.Inorganic chemistry · 2025Article
- Anticancer Potential of Azatetracyclic Derivatives: In Vitro Screening and Selective Cytotoxicity of Azide and Monobrominated Compounds.Molecules (Basel, Switzerland) · 2025Article
- Recent advances in nanoadjuvant-triggered STING activation for enhanced cancer immunotherapy.Heliyon · 2024Review
- The Influence of the Auxiliary Ligand in Monofunctional Pt(II) Anticancer Complexes on the DNA Backbone.International journal of molecular sciences · 2024Article
- Click-Capable Phenanthriplatin Derivatives as Tools to Study Pt(II)-Induced Nucleolar Stress.ACS chemical biology · 2024Article
- The Effective Synthesis of New Benzoquinoline Derivatives as Small Molecules with Anticancer Activity.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Wireframe DNA Origami for the Cellular Delivery of Platinum(II)-Based Drugs.International journal of molecular sciences · 2023Article
- Photoactive monofunctional platinum(II) anticancer complexes of multidentate phenanthridine-containing ligands: photocytotoxicity and evidence for interaction with DNA.Photochemical & photobiological sciences : Official journal of the European Photochemistry Association and the European Society for Photobiology · 2023Article
- Synthesis, Characterization, and Anticancer Activity of Phosphanegold(i) Complexes of 3-Thiosemicarbano-butan-2-one Oxime.Biomedicines · 2023Article
- Exploring the Impact of Head Group Modifications on the Anticancer Activities of Fatty-Acid-like Platinum(IV) Prodrugs: A Structure-Activity Relationship Study.International journal of molecular sciences · 2023Article
- Inhibition of nucleolar transcription by oxaliplatin involves ATM/ATR kinase signaling.Cell chemical biology · 2023Article
38 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 3 institutions in 3 countries.
Funding
Abstract
Monofunctional platinum(II) complexes of general formula cis-[Pt(NH(3))(2)(N-heterocycle)Cl]Cl bind DNA at a single site, inducing little distortion in the double helix. Despite this behavior, these compounds display significant antitumor properties, with a different spectrum of activity than that of classic bifunctional cross-linking agents like cisplatin. To discover the most potent monofunctional platinum(II) compounds, the N-heterocycle was systematically varied to generate a small library of new compounds, with guidance from the X-ray structure of RNA polymerase II (Pol II) stalled at a monofunctional pyriplatin-DNA adduct. In pyriplatin, the N-heterocycle is pyridine. The most effective complex evaluated was phenanthriplatin, cis-[Pt(NH(3))(2)(phenanthridine)Cl]NO(3), which exhibits significantly greater activity than the Food and Drug Administration-approved drugs cisplatin and oxaliplatin. Studies of phenanthriplatin in the National Cancer Institute 60-cell tumor panel screen revealed a spectrum of activity distinct from that of these clinically validated anticancer agents. The cellular uptake of phenanthriplatin is substantially greater than that of cisplatin and pyriplatin because of the hydrophobicity of the phenanthridine ligand. Phenanthriplatin binds more effectively to 5'-deoxyguanosine monophosphate than to N-acetyl methionine, whereas pyriplatin reacts equally well with both reagents. This chemistry supports DNA as a viable cellular target for phenanthriplatin and suggests that it may avoid cytoplasmic platinum scavengers with sulfur-donor ligands that convey drug resistance. With the use of globally platinated Gaussia luciferase vectors, we determined that phenanthriplatin inhibits transcription in live mammalian cells as effectively as cisplatin, despite its inability to form DNA cross-links.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.